Antibactérien

<p>MtMetAP1-IN-1 is an inhibitor of methionine aminopeptidase 1 ( MetAP1 ). MtMetAP1-IN-1 shows antimycobacterial activity.</p>

<p>BM635 mesylate inhibits MmpL3; kills Divergent bacterium with 0.6 µM MIC50; boosts bioavailability.</p>

<p>Compound 8b inhibits VEGFR-2/DHFR, combats various bacteria, and fights cancer cells.</p>

<p>PF 03709270 is an oral prodrug of sulopenem with broad-spectrum antibacterial effects on gram-positive and gram-negative bacteria.</p>

<p>Avibactam sodium dihydrate (NXL-104) is a reversible covalent inhibitor for CTX-M-15 and TEM-1 β-lactamases with IC50s of 5 nM and 8 nM.</p>

<p>7-Hydroxytropolone (3-Hydroxytropolone) is an antibiotic that exhibits activity against Gram-positive and Gram-negative bacteria, as well as yeasts and fungi. It also functions as an inhibitor of 2''-O-adenylate transferase.</p>

<p>Compound 6xa inhibits drug-resistant tuberculosis with MICs 0.03 μg/mL for DS-Mtb and 0.03-0.06 for DR-Mtb, SI&gt;40 for Vero cells.</p>

<p>Bilanafos is an agent of Anti-Bacterial.</p>

<p>AAA-10 formic is an orally active inhibitor of intestinal bacterial bile salt hydrolase (BSH) against B.</p>

<p>NDM-1 inhibitor-7 (Compound A8) is an NDM-1 inhibitor with an IC50 of 10.284 μM. It restores the ability of meropenem (MEM) to penetrate the cell wall of Gram-negative bacteria and effectively reinstates MEM's antibacterial activity against NDM-1 positive Escherichia coli. Moreover, NDM-1 inhibitor-7 demonstrates significant efficacy in both Galleria mellonella and murine peritonitis infection models.</p>

<p>KKL-40 is a small-molecule inhibitor that targets the trans-translation process, effectively suppressing methicillin-sensitive and resistant Staphylococcus aureus (S. aureus) and other Gram-positive pathogens, including vancomycin-resistant Enterococcus faecium, Bacillus subtilis, and Streptococcus pyogenes. It works in synergy with the human antimicrobial peptide LL-37 to inhibit S. aureus, but does not show synergistic effects with other antibiotics such as daptomycin, kanamycin, or erythromycin. KKL-40 inhibits trans-translation, an extreme form of recoding, while being non-toxic to HeLa cells.</p>

<p>Compound 11: Sulfonylurea derivative, antimicrobial, anticancer; MIC 0.039-0.156 mg/mL; A549 IC50: 19.7 μg/mL, PC3 IC50: 11.9 μg/mL.</p>

<p>Colistin adjuvant-1, inhibits NF-κB (IC50: 0.209 μM), boosts mucin against gram-negative bacteria.</p>

<p>β-Glucuronidase-IN-3 (Compound 49) is a covalent allosteric inhibitor targeting β-glucuronidase. It exhibits potent inhibitory activity against Escherichia coli β-glucuronidase (EcGUS) with an IC50 of 12.9 nM. The compound exerts its inhibitory effect through reversible covalent modification of cysteine residues (Cys28, Cys443, and Cys197) on EcGUS. It is applicable in research on gut microbiota-related diseases, particularly in reducing the toxic side effects of Irinotecan and non-steroidal anti-inflammatory drugs (NSAIDs).</p>

LY 215890 is a compound that exhibits potent Gram-negative and Gram-positive antibacterial activity.

MCB-3681, active against gram-positive bacterium, is the antibacterial Oxaquin's active substance.

<p>Carumonam Sodium is a monobactam, penicillin-binding protein inhibitor. It is used as antibacterials.</p>

<p>Kendomycin is a proteasome inhibitor and endothelin receptor antagonist. It induces apoptosis in lymphoma.</p>

<p>Compound 3d: antitubercular, MIC 0.007 μg/mL vs MTB H37Rv, 1.851 μg/mL vs MDR-MTB 16833, metabolically unstable.</p>

<p>Ro 24-4383 is a carbamate-linked dual-action antibacterial agent.</p>